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RECEPTORS
Vaheeda rahman, (PhD),.
Dept of pharmacology.
VISTAS
WHAT IS A RECEPTOR
RECEPTOR: It is a specific binding site on the cell which exhibits
some functional groups which trigger the
pharmacological action
AFFINITY: Ability of agent to combine with receptor
INTRINSIC ACTIVITY: Ability of agent to activate the receptor
(efficacy)
AGONIST: maximum affinity and efficacy
ANTAGONIST: having affinity but no efficacy
INVERSE AGONIST: having affinity and negative efficacy
Types of receptors:  Iono tropic receptors
 G-protein coupled receptors
 Enzymatic receptors
 Nuclear receptors
Ionotropic receptors:
G PROTEIN COUPLED RECEPTORS:
General Structure of receptors:
Structure of G-protein:
G protein coupled with receptors:
Adenyl cyclase pathway:
Step by step mechanism of G protein coupling and enzyme activation
Phospholipase C pathway:
Second messengers:
cAMP
system
Phosphoinositol
system
Arachidonic
acid system
cGMP
system
Tyrosine
kinase
system
receptor α2,β1,β2
M2
α1
M1,M3
Histamine - -
Transducer Gs(β1,β2)
Gi(α2,
M2)
Gq Unknown G-
protein
- -
Primary
effector
AC Phospholipase
C
Phospholipase
A
Guanylate
cyclase
Tyrosine
kinase
Secondary
messenger
cAMP IP3,DAG Arachidonic
acid
cGMP Protein
phosphatase
Secondary
effector
Protein
kinase A
Ca++ release 5-lipoxygenase Protein
kinase G
-
Examples of G-protein receptors:
 Muscarnic receptors (cholinergic)
 Adrenergic receptors (α,β)
 Histamine receptors
 Dopamine receptors
 Opiate receptors
 Serotonin receptors (all except 5-HT3)
 GABAB receptors
Enzymatic receptors:
Nuclear receptors:
Examples of nuclear receptors:
 Glucocorticoid receptors
 Minero corticoid receptors
 Oestrogen receptors
 Progestero receptors
 Androgen receptors
 Vit A and vit B receptors
 Thyroid hormone receptors
Other receptors:
Spare receptors: Maximum response is observed even though when all the
receptors of tissues are not occupied by drug moiety
Orphan receptors: Receptors with no endogenous ligand
Eg: PPAR-α receptors (peroxysomal proliferated activated receptors)
Silent receptors: Biologically silent even though stimulations of receptors
taking place no biological response
Normal receptors: Response observed when all the receptors of the
tissue occupied by drug moiety
REFERENCE:
 Pharmacology by RANG and DALE
 Integrated pharmacology by WALKER
 pharmacology by LIPPINCOTT
 pharmacology by BERTRUM
 www.wikkipedia.org
 www.winona.edu
 www.pharmacologycorner.com
 www.psychopharmacologyinstitute.com
Receptors

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Receptors

  • 1. RECEPTORS Vaheeda rahman, (PhD),. Dept of pharmacology. VISTAS
  • 2. WHAT IS A RECEPTOR
  • 3. RECEPTOR: It is a specific binding site on the cell which exhibits some functional groups which trigger the pharmacological action
  • 4. AFFINITY: Ability of agent to combine with receptor INTRINSIC ACTIVITY: Ability of agent to activate the receptor (efficacy) AGONIST: maximum affinity and efficacy ANTAGONIST: having affinity but no efficacy INVERSE AGONIST: having affinity and negative efficacy
  • 5.
  • 6. Types of receptors:  Iono tropic receptors  G-protein coupled receptors  Enzymatic receptors  Nuclear receptors
  • 8. G PROTEIN COUPLED RECEPTORS: General Structure of receptors:
  • 10. G protein coupled with receptors:
  • 11.
  • 13. Step by step mechanism of G protein coupling and enzyme activation
  • 15. Second messengers: cAMP system Phosphoinositol system Arachidonic acid system cGMP system Tyrosine kinase system receptor α2,β1,β2 M2 α1 M1,M3 Histamine - - Transducer Gs(β1,β2) Gi(α2, M2) Gq Unknown G- protein - - Primary effector AC Phospholipase C Phospholipase A Guanylate cyclase Tyrosine kinase Secondary messenger cAMP IP3,DAG Arachidonic acid cGMP Protein phosphatase Secondary effector Protein kinase A Ca++ release 5-lipoxygenase Protein kinase G -
  • 16. Examples of G-protein receptors:  Muscarnic receptors (cholinergic)  Adrenergic receptors (α,β)  Histamine receptors  Dopamine receptors  Opiate receptors  Serotonin receptors (all except 5-HT3)  GABAB receptors
  • 19. Examples of nuclear receptors:  Glucocorticoid receptors  Minero corticoid receptors  Oestrogen receptors  Progestero receptors  Androgen receptors  Vit A and vit B receptors  Thyroid hormone receptors
  • 20. Other receptors: Spare receptors: Maximum response is observed even though when all the receptors of tissues are not occupied by drug moiety Orphan receptors: Receptors with no endogenous ligand Eg: PPAR-α receptors (peroxysomal proliferated activated receptors) Silent receptors: Biologically silent even though stimulations of receptors taking place no biological response Normal receptors: Response observed when all the receptors of the tissue occupied by drug moiety
  • 21. REFERENCE:  Pharmacology by RANG and DALE  Integrated pharmacology by WALKER  pharmacology by LIPPINCOTT  pharmacology by BERTRUM  www.wikkipedia.org  www.winona.edu  www.pharmacologycorner.com  www.psychopharmacologyinstitute.com